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Compound Detail

CHEMBL233245

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O=C(O)c1cnnc(C2=C(c3cc(Cl)ccc3OCc3ccc(F)cc3F)CCC2)c1

Basic Information

ChEMBL ID CHEMBL233245
Phase Preclinical
Structure Type MOL
InChI Key ARMFKAHRKRNYGT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

442.9
MW (Da)
5.78
ALogP
4
HBA
1
HBD
72.3
PSA (Ų)
0.52
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H17ClF2N2O3
MW 442.85
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.07

Activity Summary

IC50 2 meas. best 8.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin E2 receptor EP1 subtype
CHEMBL1811
IC50 8.2 8.2 6.3 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.27 5.27 5400.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.kg-1 Rattus norvegicus
CL - - Rattus norvegicus
t1/2 - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prostaglandin E2 receptor EP1 subtype IC50 = 6.31 nM 8.2 Inhibition of human EP1 receptor 17084082
Cytochrome P450 2C9 IC50 = 5400.0 nM 5.27 Inhibition of human CYP2C9 17084082

Literature References

PubMed DOI Target Context # Activities
17084082 10.1016/j.bmcl.2006.10.041 Rattus norvegicus 3
17084082 10.1016/j.bmcl.2006.10.041 Prostaglandin E2 receptor EP1 subtype 1
17084082 10.1016/j.bmcl.2006.10.041 Liver microsomes 1
17084082 10.1016/j.bmcl.2006.10.041 Cytochrome P450 2C9 1
17084082 10.1016/j.bmcl.2006.10.041 No relevant target 1

Data from ChEMBL 36 via Core Engine